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Details for Patent: 4,952,579

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Details for Patent: 4,952,579

Title: Method of treating diseases by administering morpholino-ethylester of mycophenolic acid or derivatives thereof
Abstract:The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents. ##STR1##
Inventor(s): Nelson; Peter H. (Los Altos, CA), Gu; Chee-Liang L. (Synnyvale, CA), Allison; Anthony C. (Belmont, CA), Eugui; Elsie M. (Belmont, CA), Lee; William A. (Menlo Park, CA)
Assignee: Syntex (U.S.A.) Inc. (Palo Alto, CA)
Filing Date:Nov 14, 1988
Application Number:07/272,161
Claims:1. A method of treating malignant diseases in mammals, which comprises administering to a mammal suffering therewith a therapeutically effective amount of a compound represented by the formula: ##STR7## wherein: Z is hydrogen or --C(O)R, where R is lower alkyl or aryl; a a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein Z is hydrogen.

3. The method of claim 1 comprising administering an antineoplastic amount of said compound or pharmaceutically acceptable salt thereof.

4. The method of claim 2 comprising administering an antineoplastic amount of said compound or pharmaceutically acceptable salt thereof.

5. The method of claim 1 wherein said malignant disease is selected from the group: malignancies of lympho-reticular origin, and solid tumors.

6. The method of claim 5 wherein: said malignancies of lympho-reticular origin are selected from the group:

leukemias and lymphomas, including L1210 leukemia and X-5563 plastmacytoma,

human T- and B-lymphocytic and promonocytic cell line malignancies,

Burkitt lymphoma cells and other EBV-transformed B-lymphocytes, including DAUDI, CESS, SKW and malignancies corresponding thereto in humans, and T-lymphomas and leukemias including MOLT-4 and malignancies corresponding thereto in humans, and

lymphomas resulting from Epstein-Barr viral infections in allograft recipients; and

said solid tumors are selected from the group:

RIF-1 radiation-induced sarcoma, SCCVII squamous carcinoma, DIM-16 and DIM-20 mammary carcinoma, 3LL-CK Lewis lung carcinoma, NF sarcoma, sarcoma 180, and solid tumors corresponding thereto in humans.

7. The method of claim 2 wherein said malignant disease is selected from the group: malignancies of lympho-reticular origin, and solid tumors.

8. The method of claim 7 wherein: said malignancies of lympho-reticular origin are selected from the group:

leukemias and lymphomas, including L1210 leukemia and X-5563 plasmacytoma,

human T- and B-lymphocytic and promonocytic cell line malignancies,

Burkitt lymphoma cells and other EBV-transformed B-lymphocytes, including DAUDI, CESS, SKW and malignancies corresponding thereto in humans, and T-lymphomas and leukemias including MOLT-4 and malignancies corresponding thereto in humans, and

lyphomas resulting from Epstein-Barr viral infections in allograft recipients; and

said solid tumors are selected from the group:

RIF-1 radiation-induced sarcoma, SCCVII squamous carcinoma, DIM-16 and DIM-20 mammary carcinoma, 3LL-CK Lewis lung carcinoma, NF sarcoma, sarcoma 180, and solid tumors corresponding thereto in humans.
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